Isolation of potent antileishmanial agents from Artemisia kermanensis Podlech using bioguided fractionation

Abstract

Leishmaniasis is a major health problem worldwide with different clinical forms that depend on the parasite, the host's immune system, and immune-inflammatory responses. This study aimed to evaluate the secondary metabolites from Artemisia kermanensis Podlech by bioguided fractionation against Leishmania major. The chemical structures of the isolated compounds were determined based on analysis of mass and nuclear magnetic resonance spectra. Antileishmanial activity were determined on promastigotes and amastigotes. Chemical structures of the isolated compound were as 1-Acetoxy-3,7-dimethyl-7-hydroxy-octa-2E,5E-dien-4-one for compound 1 and 5,7-dihydroxy-3',4',6-trimethoxyflavone (Eupatilin) for compound 2, and 5,7,3'-Trihydroxy-6,4',5'-trimethoxyflavone for compound 3. Compound 2 were confirmed by significant activity with IC(50) of less than 50 mug/ml for 24 and 48 h in clinical form (amastigotes). Compound 3 demonstrated high susceptibility with an IC(50) of less than 30 mug/ml for promastigotes for 24 h. The bioguided fractionation of A. kermanensis resulted the isolation of potent antileishmanial agents with a low toxicity effect on macrophages. These plant metabolites can be a candidate as a drug for treating cutaneous leishmaniasis.